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Lemborexant

Cat. No. M9839
Lemborexant Structure
Synonym:

E-2006

Size Price Availability Quantity
1mg USD 110  USD110 In stock
5mg USD 230  USD230 In stock
10mg USD 420  USD420 In stock
25mg USD 760  USD760 In stock
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Quality Control & Documentation
Biological Activity

Lemborexant (E-2006) is an orally active, competitive and reversible dual OX1 and OX2 receptors antagonist, with IC50 values of 6.1 nM and 2.6 nM, respectively. Lemborexant is metabolized primarily by CYP3A4 and to a lesser extent by CYP3A5.

Chemical Information
Molecular Weight 410.42
Formula C22H20F2N4O2
CAS Number 1369764-02-2
Solubility (25°C) DMSO ≥ 90 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Carsten Theodor Beuckmann, et al. Sleep. Preclinical in vivo characterization of lemborexant (E2006), a novel dual orexin receptor antagonist for sleep/wake regulation

[2] Takashi Ueno, et al. Xenobiotica. Disposition and metabolism of [ 14 C]lemborexant, a novel dual orexin receptor antagonist, in rats and monkeys

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Keywords: Lemborexant, E-2006 supplier, OX Receptor, inhibitors, activators


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